SBI-553

SBI-553 is a beta-arrestin-biased positive allosteric modulator (PAM) of neurotensin receptor 1 (NTSR1). It binds to NSTR1 and increases neurotensin-1 affinity for NSTR1 in HEK293 cells expressing the human receptor when used at concentrations ranging from 0.01 to 10 µM. SBI-553 (0.03-30 µM) induces beta-arrestin recruitment and NTSR1 internalization without stimulating Gq protein activation, 1,4,5-triphosphate (IP3) generation, or calcium mobilization in cell-based assays. In vivo, SBI-553 (12 mg/kg, i.p.) attenuates cocaine- or methamphetamine-induced hyperlocomotion in wild-type but not beta-arrestin-2 knockout mice. It also reduces cocaine self-administration in mice.Formal Name: 2-[[2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)-1-piperidinyl]-6-quinazolinyl]methylamino]-ethanol. CAS Number: 1849603-72-0. Molecular Formula: C26H31FN4O2. Formula Weight: 450.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 3 mg/ml, DMSO: Slightly soluble, Ethanol: Slightly soluble. SMILES: FC1(CC1)C2=NC3=C(C(N4CCC(CC4)C5=C(OC)C=CC=C5)=N2)C=C(N(CCO)C)C=C3. InChi Code: InChI=1S/C26H31FN4O2/c1-30(15-16-32)19-7-8-22-21(17-19)24(29-25(28-22)26(27)11-12-26)31-13-9-18(10-14-31)20-5-3-4-6-23(20)33-2/h3-8,17-18,32H,9-16H2,1-2H3. InChi Key: BLWXTJQMEBQCIZ-UHFFFAOYSA-N.